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Alvelestat (AZD9668)

Chemical Structure : Alvelestat (AZD9668)

CAS No.: 848141-11-7

Alvelestat (AZD9668) (AZD-9668)

Catalog No.: PC-49230Not For Human Use, Lab Use Only.

Alvelestat (AZD9668, AZD-9668) is a potent, selective and orally active inhibitor of neutrophil elastase (NE) with IC50 of 12 nM, >600-fold selective over other neutrophil-derived serine proteases.

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5 mg $88 In stock
10 mg $138 In stock
25 mg $228 In stock
50 mg $388 In stock
100 mg $598 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Alvelestat (AZD9668, AZD-9668) is a potent, selective and orally active inhibitor of neutrophil elastase (NE) with IC50 of 12 nM, >600-fold selective over other neutrophil-derived serine proteases.
AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood in cell-based assays.
AZD9668 inhibited NE activity on the surface of stimulated cells and in the supernatant of primed, stimulated cells in isolated human polymorphonuclear cells.
AZD9668 showed good crossover potency to NE from other species.
Oral administration of AZD9668 to mice or rats prevented human NE-induced lung injury, measured by lung hemorrhage, and an increase in matrix protein degradation products in bronchoalveolar lavage (BAL) fluid.
AZD9668 reduced the inflammatory response to cigarette smoke as indicated by a reduction in BAL neutrophils and interleukin-1β in acute smoke models.

Physicochemical Properties

M.Wt 545.537
Formula C25H22F3N5O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-{[5-(methanesulfonyl)pyridin-2-yl]methyl}-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide

References

1. Stevens T, et al. J Pharmacol Exp Ther. 2011 Oct;339(1):313-20.

2. Kuna P, et al. Respir Med. 2012 Apr;106(4):531-9.

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